Powder: -20°C for 3 years | In solvent: -80°C for 1 year
S107 是一种 RyR 选择性 1, 4-苯并硫氮杂卓衍生物,通过增强 calstabin2 与突变和/或 PKA 磷酸化通道的结合亲和力来稳定 RyR2 通道。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 359 | 现货 | ||
2 mg | ¥ 522 | 现货 | ||
5 mg | ¥ 863 | 现货 | ||
10 mg | ¥ 1,270 | 现货 | ||
25 mg | ¥ 2,150 | 现货 | ||
50 mg | ¥ 3,190 | 现货 | ||
100 mg | ¥ 4,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 788 | 现货 |
产品描述 | S107 is a RyR-selective 1, 4-benzothiazepine derivative that stabilizes RyR2 channels by enhancing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels. |
体外活性 | S107 is a small compound that enhances calstabin2 binding to RyR2 at low nanomolar concentrations and failed to interact with over 400 receptors, enzymes, and ion channels in screens using up to 10 μM of the compound. S107 has no effect on cardiac ion channels including the voltage-gated Na+, K+, and Ca2+ channels at concentrations up to 10 μM, and S107 had no effect on normal Ca2+ signaling in cells[1]. S107 is a promising candidate drug for treating catecholaminergic polymorphic ventricular tachycardia (CPVT). S107 exerts an antiarrhythmic effect on CPVT-hiPSC-CMs. Pre-incubation with 10 μM S107, which stabilizes the closed state of the ryanodine receptor 2, significantly decreases the percentage of CPVT-hiPSC-CMs presenting DADs to 25%[2]. S107 is thought to improve skeletal muscle function by stabilizing the RyR1-FKBP12 complex. S107 increases FKBP12 binding to RyR1 in SR vesicles in the presence of reduced glutathione and the NO-donor NOC12, with no effect in the presence of oxidized glutathione. S107 can reverse the harmful effects of redox active species on SR Ca2+ release in skeletal muscle by binding to RyR1 low affinity sites[3]. |
体内活性 | S107可防止通道漏失,但不封锁通道或改变正常的Ca2+信号传导,能够在突变小鼠中抑制癫痫发作和心律失常[1]。 |
分子量 | 209.31 |
分子式 | C11H15NOS |
CAS No. | 927871-76-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (262.77 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.7776 mL | 23.888 mL | 47.776 mL | 119.4401 mL |
5 mM | 0.9555 mL | 4.7776 mL | 9.5552 mL | 23.888 mL | |
10 mM | 0.4778 mL | 2.3888 mL | 4.7776 mL | 11.944 mL | |
20 mM | 0.2389 mL | 1.1944 mL | 2.3888 mL | 5.972 mL | |
50 mM | 0.0956 mL | 0.4778 mL | 0.9555 mL | 2.3888 mL | |
100 mM | 0.0478 mL | 0.2389 mL | 0.4778 mL | 1.1944 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
S107 927871-76-9 Others S 107 S-107 Inhibitor inhibitor inhibit